WS6 是一种具有促beta细胞增生作用的新型小分子,在啮齿类动物和人源原发性胰岛中EC50值为0.28uM。
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描述
WS6, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
体外活性
在切除β细胞的RIP-DTA小鼠模型中,给口服WS6(50 mg/kg )能够β细胞增殖,从而改善糖尿病.
体内活性
在R7T1细胞中(EC50=0.28 μM),WS6通过Erb3结合蛋白-1和IκB激酶信号通路作用,诱导细胞增殖。
激酶实验
PARP assays are conducted in a buffer containing 50 mM Tris (pH 8.0), 1 mM DTT, 1.5 μM [3H]NAD+?(1.6 μCi/mmol), 200 nM biotinylated histone H1, 200 nM slDNA, and 1 nM PARP-1 or 4 nM PARP-2 enzyme. Reactions are terminated with 1.5 mM benzamide, transferred to streptavidin Flash plates, and counted using a TopCount microplate scintillation counter.
细胞实验
R7T1 cells are growth-arrested by removal of doxycycline for 2 days and plated into 384-well plates at a density of 3,000 cells/well in growth medium. Β cell proliferation is assessed using CellTiter Glo after 4 days. Fold increase in cell number is calculated by normalizing compound-treated wells to the median of DMSO-treated wells. (Only for Reference)
Cas No.
1421227-53-3
分子式
C29H31F3N6O3
分子量
568.601
储存和溶解度
Ethanol:93 mg/mL (163.6 mM)
DMSO:93 mg/mL (163.6 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years